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TD52

Catalog No. T35528Cas No. 1798328-24-1

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

TD52

TD52

Catalog No. T35528Cas No. 1798328-24-1
TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.
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Product Introduction

Bioactivity
Description
TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.
In vitro
TD52 (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells. TD52 (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2. TD52 (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines. TD52 (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression. TD52 (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt[1].
In vivo
In female NCr athymic nude mice, TD52 (10 mg/kg/day; oral gavage) significantly inhibited MDA-MB-468 xenograft tumour size and tumour weight and decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours.[1].
Chemical Properties
Molecular Weight360.41
FormulaC24H16N4
Cas No.1798328-24-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 95 mg/mL (263.59 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7746 mL13.8731 mL27.7462 mL138.7309 mL
5 mM0.5549 mL2.7746 mL5.5492 mL27.7462 mL
10 mM0.2775 mL1.3873 mL2.7746 mL13.8731 mL
20 mM0.1387 mL0.6937 mL1.3873 mL6.9365 mL
50 mM0.0555 mL0.2775 mL0.5549 mL2.7746 mL
100 mM0.0277 mL0.1387 mL0.2775 mL1.3873 mL

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